Description
AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases.
Product information
CAS Number: 2247950-42-9
Molecular Weight: 441.50
Formula: C25H24FN7
Chemical Name: (3R)-N-[2-(5-fluoropyridin-3-yl)-8-(propan-2-yl)pyrazolo[1, 5-a][1, 3, 5]triazin-4-yl]-2, 3, 4, 9-tetrahydro-1H-carbazol-3-amine
Smiles: CC(C)C1C=NN2C=1N=C(N=C2N[C@@H]1CCC2NC3=CC=CC=C3C=2C1)C1=CN=CC(F)=C1
InChiKey: QPFPBVPZIIDXGT-QGZVFWFLSA-N
InChi: InChI=1S/C25H24FN7/c1-14(2)20-13-28-33-24(20)31-23(15-9-16(26)12-27-11-15)32-25(33)29-17-7-8-22-19(10-17)18-5-3-4-6-21(18)30-22/h3-6,9,11-14,17,30H,7-8,10H2,1-2H3,(H,29,31,32)/t17-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
AHR antagonist 5 free base (Compound A) potently inhibits AHR activity in human and rodent cell lines (IC50 of ~35-150 nM). In human T cell assays, AHR antagonist 5 free base induces an activated T cell state. AHR antagonist 5 free base inhibits CYP1A1 and interleukin (IL)-22 gene expression and leads to an increase in pro-inflammatory cytokines, such as IL-2 and IL-9.
In Vivo:
AHR antagonist 5 free base (Compound A) has been evaluated in a series of pharmacological, single-dose and repeated-dose toxicological studies in rodent and non-rodent species including 28-day Good Laboratory Practice (GLP) studies in rat and monkeys. All changes are resolved or resolving after 2 weeks of dosing cessation, except for the testicular changes in rats.
Products are for research use only. Not for human use.
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